CN101874790A - Orally disintegrating tablet of Rasagiline or medicine salts thereof and preparation method thereof - Google Patents
Orally disintegrating tablet of Rasagiline or medicine salts thereof and preparation method thereof Download PDFInfo
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- CN101874790A CN101874790A CN2009100150012A CN200910015001A CN101874790A CN 101874790 A CN101874790 A CN 101874790A CN 2009100150012 A CN2009100150012 A CN 2009100150012A CN 200910015001 A CN200910015001 A CN 200910015001A CN 101874790 A CN101874790 A CN 101874790A
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Abstract
The invention belongs to the technical field of medicines and relates to an orally disintegrating tablet of Rasagiline or medicine salts thereof and a preparation method thereof. The orally disintegrating tablet comprises the following components in percentage by weight: 0.25-2 percent of Rasagiline or medicine salts thereof, 85-91 percent of spray drying mannitol, 3-10 percent of disintegrant, 0.5-2 percent of flow agent, 0.5-2 percent of lubricant, 0-2 percent of sweetener and 0-2 percent of flavoring agent. The raw materials and the auxiliary materials are uniformly mixed to obtain uniform fine powder which is directly squashed to form tablets. The orally disintegrating tablet of the Rasagiline or the medicine salts thereof has enough hardness, can satisfy the requirements of production, packaging, storage and transportation and also has good taste and shorter disintegration time.
Description
Technical field
The present invention relates to a kind of rasagiline of Parkinson disease or oral cavity disintegration tablet of its pharmaceutical salts and preparation method thereof for the treatment of, belong to medical technical field.
Background technology
National drug evaluate the center will be in the oral cavity tablet of disintegrate fast (or dissolving), unified Definition is " oral cavity disintegration tablet (0rally disintegrating tablets) ".Oral cavity disintegration tablet does not need the water can disintegrate in the oral cavity, when taking, this product is placed lingual surface, need not use water delivery service, this product disintegrate and swallow into stomach with saliva voluntarily.
The technology of preparing of oral cavity disintegration tablet mainly is divided into two big classes: lyophilization and pressed disc method.Freeze-dry orally disintegrating tablet is generally used vacuum freeze-drying method, adopts the solubility adjuvant to prepare, and its disintegration rate has surpassed the oral cavity disintegration tablet (30 seconds) of pressed disc method preparation, and drug effect is faster, does not have grittiness, and mouthfeel is more refreshing.Abroad main employing at present is lyophilization, and this technology has also had quantum Gao Ke group to adopt at present at home.But the lyophilization production cost is higher, and technical difficulty is big, the equipment complexity, and need special blister package further increase its cost because the product friability is high.Pressed disc method prepares oral cavity disintegration tablet is by adopting the fine but undissolved adjuvant of disintegrative, suppresses out by common tablet machine, and its advantage is, can utilize existing oral solid formulation Workshop Production, technical difficulty is little, small investment, technology is simple, and cost is low, but second-rate.Owing to be to use insoluble adjuvant, there is sand to press against sense, the taste of adjuvant is not tasty and refreshing yet, so its mouthfeel is relatively poor.
Parkinson disease can make the patient dysphagia (Potulska occur, A., A.Friedman, et a1. (2003). " Swallowingdisorders in Parkinson ' s disease. " Parkinsonism and Related Disorders 9 (6): 349-353.), be difficult to normally take conventional tablet or capsule, and the characteristics of oral cavity disintegration tablet help to overcome this difficulty, can effectively improve the compliance that the patient takes medicine.
Therefore, seek a kind of adopt the enough hardness of having of common sheeting equipment and prepared and can disintegrate fast in the oral cavity, rasagiline or its pharmaceutical salts oral cavity disintegration tablet that mouthfeel is good be highly significant.
Chinese patent CN1476826 (application number 03149856.6) " oral cavity disintegration tablet and preparation method thereof ", adopt mannitol, lactose, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone etc., prepare oral cavity disintegration tablet with pressed disc method, disintegration time was less than 20 seconds.
Chinese patent CN1658838 (application number 03813525.6) " oral cavity disintegration tablet and preparation method thereof ", adopt mannitol, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose and lubricant, the consumption of microcrystalline Cellulose is between 10～18% in wherein writing out a prescription, prepare oral cavity disintegration tablet with pressed disc method, external disintegration time was less than 40 seconds.
Chinese patent CN1613442 (application number 200310108459.5) " a kind of oral cavity disintegration tablet of effective taste masking and preparation method ", adopt resin or cellulose family adjuvant that the principal agent composition is wrapped up, add mannitol, lactose, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose or polyvinylpolypyrrolidone etc. then, prepare oral cavity disintegration tablet with pressed disc method, disintegration time was less than 45 seconds.
Chinese patent CN1787811 (application number 200480013099.3) " oral cavity disintegration tablet " has adopted silicified microcrystalline cellulose to prepare oral cavity disintegration tablet as disintegrating agent, and disintegration time is less than less than 60 seconds.
All adopted microcrystalline Cellulose or low-substituted hydroxypropyl cellulose in the above-mentioned prescription, the application of such adjuvant causes producing sense of discomfort after its disintegrate in the oral cavity.And adopt technique for packing to prepare oral cavity disintegration tablet, complex production process, productive rate is low.
Chinese patent CN108098685A (application number 200580046326.7) provides the preparation method of preparation rasagiline or its pharmaceutical salts oral cavity disintegration tablet, but the sodium stearyl fumarate that adopts in this method does not still have the authentication code of State Food and Drug Administration; The sorbitol hygroscopicity height of using in this patent simultaneously is unfavorable for the preservation of oral cavity disintegration tablet, and sorbitol has bigger eye zest, needs in the production to strengthen protection, has limited its application in actual pharmaceuticals industry.According to this patent specification, when the tablet that its embodiment makes carries out disintegrating method in the method that adopts the USP regulation, surpass 30 seconds disintegration, do not meet oral cavity disintegration tablet that FDA recommends and adopt USP disintegration time mensuration method disintegration time less than 30 seconds requirement.Evaluate " the oral cavity disintegration tablet guideline draft and the discussion of FDA issue " that published on May 8th, 2007 at the center according to State Food and Drug Administration's medicine, China's oral cavity disintegration tablet key Quality Control requires the said preparation product, and disintegration time should be less than 1 minute in less than 37 ℃ the water of 2ml, and the described method of Chinese patent CN108098685A (application number 200580046326.7) is difficult to reach this requirement.
In sum, though above-mentioned content all discloses the method for making of oral cavity disintegration tablet and application etc., but at rasagiline or its pharmaceutical salts oral cavity disintegration tablet, also be not fit to actual product that uses and operate of China and method for making, in the disclosed preparation method of above-mentioned Chinese patent CN108098685A, also exist deficiency simultaneously.
Summary of the invention
The present invention is directed to the deficiencies in the prior art, the oral cavity disintegration tablet of a kind of rasagiline or its pharmaceutical salts is provided, and adopt common press device and simple process to prepare the method for rasagiline or its pharmaceutical salts oral cavity disintegration tablet, and the adjuvant that adopts in this method is the pharmaceutic adjuvant of State Food and Drug Administration's approval, results of stability shows that the rasagiline of the present invention's preparation or its pharmaceutical salts oral cavity disintegration tablet have stability preferably, can be applied to actual pharmaceuticals industry production.This rasagiline or its pharmaceutical salts oral cavity disintegration tablet have enough hardness, can satisfy the requirement of production, packing, accumulating, have good mouthfeel and short disintegration time simultaneously again.
Technical scheme of the present invention is as follows: adopt spray drying mannitol as filler, its consumption mark is by weight counted: 85～91%.
Rasagiline or its pharmaceutical salts oral cavity disintegration tablet, by weight percentage, concrete composition is as follows:
Rasagiline or its pharmaceutical salts 0.25～2%
Spray drying mannitol 85～91%
Disintegrating agent 3～10%
Fluidizer 0.5～2%
Lubricant 0.5～2%
Sweeting agent 0～2%
Correctives 0～2%
For guaranteeing rasagiline or the quick stripping of its pharmaceutical salts oral cavity disintegration tablet, the present invention is as follows to the granularity requirements of above-mentioned rasagiline: the rasagiline of at least 90% weight or its pharmaceutical salts have the granularity that is lower than 120 μ m, and preferably the rasagiline of at least 90% weight or its pharmaceutical salts have the granularity that is lower than 75 μ m.
Described spray drying mannitol is (as French Roquette Freres
) have and make it become the ideal physicochemical properties of forming suitable filler of the present invention, Chinese patent file CN1658838 (application number 03813525.6) describes in detail, its good fluidity, compressibility height, its sweet taste ability is about 50% of sucrose, the characteristic of its negative heat of solution can be brought better organoleptic properties, clean taste.The oral cavity disintegration tablet that adopts this method to prepare simultaneously meets requirement disintegration under the oral cavity disintegration tablet disintegration time assay method that adopts State Food and Drug Administration's medicine to evaluate the center proposition.A series of problems of rasagiline described in the Chinese patent CN108098685A and pharmaceutical salts Orally disintegrating piece preparation method thereof have been solved.
By long-term creative research, the present invention has determined that rasagiline or its pharmaceutical salts oral cavity disintegration tablet must comprise the spray drying mannitol of 85～91% weight; Such weight ratio can make the weigh requirement of pharmacopeia regulation of the sheet of the rasagiline made or its pharmaceutical salts oral cavity disintegration tablet, reaches ideal drug effect simultaneously.
Described disintegrating agent is cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone and carboxymethyl starch sodium, is preferably wherein any two kinds of use in conjunction jointly as disintegrating agent.
The selection of described disintegrating agent is most important for oral cavity disintegration tablet.Find that by comparative study select microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone coupling as disintegrating agent, though disintegration rate increases, product has grittiness, mouthfeel is not good.And the oral cavity disintegration tablet disintegration time of single disintegrating agent preparation was long than the two coupling disintegration time, above 60 seconds.The disintegrating agent that the present invention selects is cross-linking sodium carboxymethyl cellulose and carboxymethyl starch sodium or polyvinylpolypyrrolidone and carboxymethyl starch sodium, and Neither of the two can be dispensed; Adopt this combination both can obtain satisfied disintegration time (less than 30 seconds), the mouthfeel when not influencing disintegration of tablet simultaneously.
The ratio of described cross-linking sodium carboxymethyl cellulose in rasagiline or its pharmaceutical salts oral cavity disintegration tablet is preferably 1～4% of tablet total weight amount, more preferably 2～3%, the excessive cross-linking sodium carboxymethyl cellulose that uses in prescription not only can not improve disintegration rate, and influences the mouthfeel of prepared oral cavity disintegration tablet; Same reason, the percentage by weight of technology controlling and process polyvinylpolypyrrolidone is 1～4%, is preferably 2～3%.
The ratio of described carboxymethyl starch sodium in rasagiline or its pharmaceutical salts oral cavity disintegration tablet is preferably 2～6% of tablet total weight amount, and more preferably 4～5%.
Rasagiline of the present invention or its pharmaceutical salts oral cavity disintegration tablet be the fine powder direct compression preferably, for increasing its flowability, must add a certain amount of fluidizer in the prescription, preferred fluidizer is micropowder silica gel, its ratio should be 0.5～2% weight of tablet total weight amount, in addition also can adopt other fluidizer commonly used on the market.
For preventing sticking in the tabletting process, guarantee smooth slice, must add lubricant.The lubricant that adopts in this method is magnesium stearate and stearic acid, by stability study find stearic acid and rasagiline with and the compatibility of pharmaceutical salts rasagiline mesilate better, therefore lubricant is preferably stearic acid, its ratio should be 0.5～2% weight of tablet total weight amount, in addition also can adopt other lubricants commonly used on the market.
For making the patient obtain better mouthfeel in the oral cavity disintegration tablet that uses this law preparation, tablet of the present invention can also comprise sweet taste/flavoring system, and sweeting agent can be selected aspartame, saccharin sodium or stevioside etc.; Correctives can be selected Oleum menthae or fruit essence etc.; Each component ratio should be 0～2% weight of tablet total weight amount.
The preparation method of above-mentioned rasagiline or its pharmaceutical salts oral cavity disintegration tablet is as follows:
Rasagiline or its pharmaceutical salts, spray drying mannitol, disintegrating agent, fluidizer, lubricant are mixed in proportion, also can suitably add sweeting agent, correctives; Mix homogeneously with the fine powder direct compression, promptly gets rasagiline or its pharmaceutical salts oral cavity disintegration tablet.
For guaranteeing the quick stripping of rasagiline in above-mentioned rasagiline or its pharmaceutical salts oral cavity disintegration tablet or its pharmaceutical salts, before preparation, raw material is carried out pretreatment, processing method is as follows:
Rasagiline or its pharmaceutical salts raw material are carried out pulverization process, adopt the laser particle size detector to detect its granularity, make the rasagiline of at least 90% weight or its pharmaceutical salts have the granularity that is lower than 120 μ m.
The present invention prepares rasagiline or its pharmaceutical salts oral cavity disintegration tablet of confession, the heavy 70-200mg of monolithic, and hardness 2.5-4kg, friability 0.1-0.5%, disintegration time is less than 30 seconds.
The present invention prepares satisfactory oral cavity disintegration tablet by adopting spray drying mannitol as the tablet skeleton in sum.Make the support skeleton of porous particles with spray-dired method as tablet, after the oral cavity disintegration tablet made from direct compressions such as solubilizing agent and extender, filler, correctivess is met saliva, moisture can enter the tablet inner core rapidly, can obtain quickly disintegrated effect owing to the repulsion of same sex electrostatic charge in the granule, mannitol can bring extraordinary mouthfeel simultaneously, increases patient's compliance.
The present invention selects good filler and disintegrating agent for use, and the rasagiline or its pharmaceutical salts oral cavity disintegration tablet that adopt appropriate simple preparation process to make, disintegrate rapidly behind the tablet inlet, and its disintegration time is 5-30 second.With water is dissolution medium, and stripping in 15 minutes is more than 85%.Accelerated test result shows, this oral cavity disintegration tablet accelerated test 6 months, steady quality.
The specific embodiment
Following examples only are used to further specify the present invention, but do not limit the present invention.
Test method and test instrunment are as follows among the embodiment:
A, hardness measurement instrument: YD-1 tablet hardness tester (Tianjin state inscription medical equipment company limited)
Get rasagiline or 10 of its pharmaceutical salts oral cavity disintegration tablets (n=10), survey tablet hardness with YD-1 tablet hardness tester respectively, average.
B, disintegration time mensuration adopt static disintegrate method.Get 1 of rasagiline or its pharmaceutical salts oral cavity disintegration tablet, put in the 10ml test tube (the test tube internal diameter is 13mm), in vitro fill 2ml water, water temperature is 37 ℃, and tablet should disintegrate in 1 minute, be dispersed in the water.Pour out and sieve, each water 2ml, wash test tube and screen cloth at twice, can be all by the screen cloth of aperture less than 710 μ m.Check 6 (n=6) as stated above, should be up to specification.
C, intraoral disintegration time limit and mouthfeel
10 healthy volunteers adopt placebo to carry out the intraoral disintegration test.Measure intraoral disintegration time limit and mouthfeel.
D. friability is measured, and tests according to Chinese Pharmacopoeia version appendix in 2005 X G tablet friability inspection technique.
Embodiment 1:
Rasagiline or its pharmaceutical salts oral cavity disintegration tablet composed as follows:
| Supplementary material | The mg/ sheet | %/sheet |
| Rasagiline mesilate | ??0.25 | ??0.36 |
| Spray drying mannitol | ??62.4 | ??89.14 |
| Cross-linking sodium carboxymethyl cellulose | ??2.8 | ??4 |
| Carboxymethyl starch sodium | ??1.4 | ??2 |
| Oleum menthae | ??1.4 | ??2 |
| Micropowder silica gel | ??0.35 | ??0.5 |
| Supplementary material | The mg/ sheet | %/sheet |
| Stearic acid | ??1.4 | ??2 |
| Sheet is heavy | ??70 | ??100 |
With the former abrasive lapping of rasagiline mesilate, cross 100 mesh sieves, standby.After getting recipe quantity rasagiline mesilate and each adjuvant mix homogeneously, being pressed into diameter is 6mm circular flat sheet.
Result of the test:
A, hardness measurement (YD-1 tablet hardness tester) result: meansigma methods 3.5 ± 0.5Kg (n=10).
B, disintegration time mensuration result: 5～15 seconds (n=6)
C, intraoral disintegration time limit and mouthfeel
10 healthy volunteers, measurement result: disintegrate in 15 seconds, no grittiness and sense of discomfort, little sweet.
Embodiment 2:
Rasagiline or its pharmaceutical salts oral cavity disintegration tablet composed as follows:
| Supplementary material | The mg/ sheet | %/sheet |
| Rasagiline | ??0.5 | ??0.5 |
| Spray drying mannitol | ??91 | ??91 |
| Cross-linking sodium carboxymethyl cellulose | ??2 | ??2 |
| Carboxymethyl starch sodium | ??4 | ??4 |
| Micropowder silica gel | ??2 | ??2 |
| Magnesium stearate | ??0.5 | ??0.5 |
| Sheet is heavy | ??100 | ??100 |
Behind each raw material mix homogeneously, be pressed into the circular two-sided convex sheet of diameter 7mm.
Hardness meansigma methods 3.5 ± 0.5Kg (n=10).
Disintegration time mensuration result: 5～15 seconds (n=6)
Embodiment 3:
Rasagiline or its pharmaceutical salts oral cavity disintegration tablet composed as follows:
| Supplementary material | The mg/ sheet | %/sheet |
| Rasagiline mesilate | ??1 | ??0.74 |
| Spray drying mannitol | ??117.8 | ??87.26 |
| Cross-linking sodium carboxymethyl cellulose | ??4.05 | ??3 |
| Carboxymethyl starch sodium | ??6.75 | ??5 |
| Micropowder silica gel | ??2.7 | ??2 |
| Stearic acid | ??2.7 | ??2 |
| Sheet is heavy | ??135 | ??100 |
Behind each component mix homogeneously of raw material, be pressed into the circular two-sided spill sheet of diameter 8mm.
Hardness meansigma methods 3 ± 0.5Kg (n=10).
Disintegration time mensuration result: 15～25 seconds (n=6)
Friability is less than 0.5%.
Dissolution: stripping in 10 minutes is more than 95% (n=6).
Uniformity of dosage units: up to specification.
Accelerated test 6 months, every quality index is stable.The results are shown in following table:
Embodiment 4:
Rasagiline or its pharmaceutical salts oral cavity disintegration tablet composed as follows:
| Supplementary material | The mg/ sheet | %/sheet |
| Rasagiline | ??2 | ??1 |
| Supplementary material | The mg/ sheet | %/sheet |
| Spray drying mannitol | ??174 | ??87 |
| Cross-linking sodium carboxymethyl cellulose | ??6 | ??3 |
| Carboxymethyl starch sodium | ??10 | ??5 |
| Flavoring orange essence | ??1 | ??0.5 |
| Micropowder silica gel | ??3 | ??1.5 |
| Magnesium stearate | ??4 | ??2 |
| Sheet is heavy | ??200 | ??100 |
Behind the supplementary material mix homogeneously, be pressed into the circular two-sided spill sheet of diameter 9mm.
Hardness meansigma methods 3 ± 0.5Kg (n=10).
Disintegration time mensuration result: 10～30 seconds (n=6)
Friability is less than 0.5%.
Embodiment 5:
Rasagiline or its pharmaceutical salts oral cavity disintegration tablet composed as follows:
| Supplementary material | The mg/ sheet | %/sheet |
| Rasagiline | ??0.25 | ??0.36 |
| Spray drying mannitol | ??62.4 | ??89.14 |
| Polyvinylpolypyrrolidone | ??2.8 | ??4 |
| Carboxymethyl starch sodium | ??1.4 | ??2 |
| Oleum menthae | ??1.4 | ??2 |
| Micropowder silica gel | ??0.35 | ??0.5 |
| Stearic acid | ??1.4 | ??2 |
| Sheet is heavy | ??70 | ??100 |
With the former abrasive lapping of rasagiline, cross 180 mesh sieves, standby.After getting recipe quantity rasagiline and each adjuvant mix homogeneously, being pressed into diameter is 6mm circular flat sheet.
Result of the test:
A, hardness measurement (YD-1 tablet hardness tester) result: meansigma methods 3.5 ± 0.5Kg (n=10).
B, disintegration time mensuration result: 5～15 seconds (n=6)
Comparative example
We have carried out the contrast experiment according to the described method of Chinese patent CN108098685A (application number 200580046326.7), and are composed as follows:
Form 1 Chinese patent CN108098685A test recipe forms 1
Form 2 Chinese patent CN108098685A test recipes form 2
Tablet forming technique: the mixing of will the adjuvant equivalent except that lubricant progressively increasing, cross 60 order stainless steel meshs 5 times after the airbag mode of averaging mixed 3 minutes, add after lubricant is crossed 60 order stainless steel meshs, the airbag mode of averaging mixed 1 minute.According to the heavy direct compression of sheet that corresponding prescription is formed, regulate the tablet that tablet machine pressure makes different hardness.
The disintegrating method method: add 37 ℃ hot water 2ml in the 10ml test tube, drop into tablet to be measured gently, pick up counting simultaneously, the complete disintegration time of observed and recorded tablet stops measuring when 1min, observes whether disintegrate fully of tablet.
Result of the test: the test recipe according to Chinese patent CN108098685A preparation is formed 1 tablet under 5.7kg hardness and 2.4kg hardness, and requiring all according to Chinese oral cavity disintegration tablet key Quality Control can not disintegrate fully in 1min; Test recipe according to Chinese patent CN108098685A preparation is formed 2 tablets under 4.8kg hardness and 1.6kg hardness, and requiring according to Chinese oral cavity disintegration tablet key Quality Control all can not disintegrate fully in 1min.
By above-mentioned experiment as can be known, be difficult to reach the state food and drug administration medicine according to the oral cavity disintegration tablet of Chinese patent CN108098685A preparation and evaluate " the oral cavity disintegration tablet guideline draft and the discussion of FDA issue " that published on May 8th, 2007 at the center, China's oral cavity disintegration tablet key Quality Control requirement, and according to the prepared rasagiline oral cavity disintegration tablet of technical solution of the present invention (embodiment 1-5) disintegrate fully in 30 seconds, meet this requirement fully, be suitable for applying widely.
Claims (9)
1. the oral cavity disintegration tablet of a rasagiline or its pharmaceutical salts is characterized in that: adopt spray drying mannitol as filler, its consumption mark is by weight counted: 85～91%.
2. oral cavity disintegration tablet according to claim 1 is characterized in that: each composition is as follows by weight percentage:
Rasagiline or its pharmaceutical salts 0.25～2%
Spray drying mannitol 85～91%
Disintegrating agent 3～10%
Fluidizer 0.5～2%
Lubricant 0.5～2%
Sweeting agent 0～2%
Correctives 0～2%.
3. oral cavity disintegration tablet according to claim 1 and 2 is characterized in that: the pharmaceutical salts of described rasagiline is a rasagiline mesilate.
4. oral cavity disintegration tablet according to claim 1 and 2, it is characterized in that: its granularity of part of at least 90% weight fraction is lower than 120 μ m in described rasagiline or its pharmaceutical salts, and the rasagiline of preferred at least 90% weight has the granularity that is lower than 75 μ m.
5. the oral cavity disintegration tablet of rasagiline according to claim 2 or its pharmaceutical salts is characterized in that: described disintegrating agent is cross-linking sodium carboxymethyl cellulose and carboxymethyl starch sodium or polyvinylpolypyrrolidone and carboxymethyl starch sodium; Described fluidizer is micropowder silica gel; Described lubricant is a stearic acid.
6. rasagiline according to claim 5 or its pharmaceutical salts oral cavity disintegration tablet, it is characterized in that: the percentage by weight of cross-linking sodium carboxymethyl cellulose is 1～4%, is preferably 2～3%; The percentage by weight of polyvinylpolypyrrolidone is 1～4%, is preferably 2～3%; The percentage by weight of carboxymethyl starch sodium is 2～6%, is preferably 4～5%.
7. oral cavity disintegration tablet according to claim 1 and 2, it is characterized in that: described rasagiline or its pharmaceutical salts oral cavity disintegration tablet, the heavy 70-200mg of monolithic, hardness 2.5-4kg, friability 0.1-0.5%, the disintegration time that adopts static disintegration time mensuration method to measure is 10-30 second.
8. prepare the preparation method of rasagiline according to claim 1 or its pharmaceutical salts oral cavity disintegration tablet, it is characterized in that: step is as follows:
Rasagiline or its pharmaceutical salts, spray drying mannitol, disintegrating agent, fluidizer, lubricant are mixed in proportion, add sweeting agent, correctives, mix homogeneously; The even fine powder direct compression that will obtain then prepares the oral cavity disintegration tablet of rasagiline or its pharmaceutical salts.
9. the preparation method of rasagiline according to claim 8 or its pharmaceutical salts oral cavity disintegration tablet is characterized in that: handle as follows for the effective ingredient rasagiline in the raw material or its pharmaceutical salts:
Rasagiline or its pharmaceutical salts raw material are carried out pulverization process, adopt the laser particle size detector to detect its granularity, its granularity of part that makes its granularity reach at least 90% weight fraction is lower than 120 μ m.
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| Application Number | Priority Date | Filing Date | Title |
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| CN2009100150012A CN101874790B (en) | 2009-04-29 | 2009-04-29 | Orally disintegrating tablet of Rasagiline or medicine salts thereof and preparation method thereof |
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| CN2009100150012A CN101874790B (en) | 2009-04-29 | 2009-04-29 | Orally disintegrating tablet of Rasagiline or medicine salts thereof and preparation method thereof |
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| CN101874790B CN101874790B (en) | 2012-06-06 |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109152841A (en) * | 2016-03-26 | 2019-01-04 | 雷迪博士实验室有限公司 | The pharmaceutical composition of N- propargylamine derivative |
| WO2022083063A1 (en) | 2020-10-23 | 2022-04-28 | 上海上药中西制药有限公司 | Sublingual film dosage of rasagiline or pharmaceutically acceptable salt thereof, and preparation method therefor and use thereof |
| CN114668732A (en) * | 2022-02-24 | 2022-06-28 | 浙江和泽医药科技股份有限公司 | Bepotastine besilate orally disintegrating tablet and preparation method thereof |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4035654A1 (en) * | 2021-01-30 | 2022-08-03 | Intas Pharmaceuticals Limited | An orodispersible pharmaceutical solid dosage form of rasagiline |
| WO2022162612A1 (en) * | 2021-01-30 | 2022-08-04 | Intas Pharmaceuticals Ltd. | An orodispersible pharmaceutical solid dosage form of rasagiline |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020071864A1 (en) * | 1999-03-25 | 2002-06-13 | Yuhan Corporation | Rapidly disintegrable tablet for oral administration |
| ES2199061B1 (en) * | 2002-06-10 | 2005-02-16 | Laboratorios Vita, S.A. | TROUBLE-BASED TABLETS AND PROCEDURE FOR OBTAINING. |
| CN101098685A (en) * | 2004-11-24 | 2008-01-02 | 特瓦制药工业有限公司 | Rasagiline orally disintegrating compositions |
-
2009
- 2009-04-29 CN CN2009100150012A patent/CN101874790B/en active Active
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109152841A (en) * | 2016-03-26 | 2019-01-04 | 雷迪博士实验室有限公司 | The pharmaceutical composition of N- propargylamine derivative |
| WO2022083063A1 (en) | 2020-10-23 | 2022-04-28 | 上海上药中西制药有限公司 | Sublingual film dosage of rasagiline or pharmaceutically acceptable salt thereof, and preparation method therefor and use thereof |
| CN114668732A (en) * | 2022-02-24 | 2022-06-28 | 浙江和泽医药科技股份有限公司 | Bepotastine besilate orally disintegrating tablet and preparation method thereof |
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| Publication number | Publication date |
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| CN101874790B (en) | 2012-06-06 |
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